Tertiapin-Q. A Potent Blocker of some Inward Rectifier�(Kir)�K+�Channels.
The native toxin Tertiapin was originally isolated from�European�honey bee�Apis mellifera�venom.��Native and synthetic Tertiapin blocks a range of inward rectifier K+channels (Kir),�in particular ROMK1 (Kir1.1, IC50=2 nM) and GIRK (Kir3 family, IC50�for the�Kir3.1/3.4 heteromer was 8.6 nM) but with no effect on Kir2 family member.�In accordance, it was shown to inhibit acetylcholine induced K+�currents in�mammalian cardiomyocytes.
Tertiapin-Q is a derivative of Tertiapin in which Met13�is�substituted�by Gln residue. However, unlike native Tertiapin, Tertiapin-Q is non-oxidizable and therefore is more stable.
Tertiapin-Q inhibits the above-mentioned channels with similar affinities and also�inhibits Ca2�activated large conductance BK-type K+�channels in a concentration, and voltage-dependent manner.
Alomone Labs is pleased to offer Tertiapin-Q,�a purified synthetic peptide�in economical sizes�and at�very attractive prices.
Ion Channel Modulators; K+ Channel Blockers